JP2012503621A5 - - Google Patents
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- Publication number
- JP2012503621A5 JP2012503621A5 JP2011528309A JP2011528309A JP2012503621A5 JP 2012503621 A5 JP2012503621 A5 JP 2012503621A5 JP 2011528309 A JP2011528309 A JP 2011528309A JP 2011528309 A JP2011528309 A JP 2011528309A JP 2012503621 A5 JP2012503621 A5 JP 2012503621A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- allyl
- halogen
- compound according
- alkoxy
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 3
- -1 alkylene diol Chemical class 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 239000003080 antimitotic agent Substances 0.000 claims 1
- 230000006907 apoptotic process Effects 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 150000005846 sugar alcohols Polymers 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08165147.3 | 2008-09-25 | ||
| EP08165147A EP2174947A1 (en) | 2008-09-25 | 2008-09-25 | Bioactive pre-tubulysins and use thereof |
| PCT/EP2009/062282 WO2010034724A1 (en) | 2008-09-25 | 2009-09-22 | Bioactive pre-tubulysins and use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012503621A JP2012503621A (ja) | 2012-02-09 |
| JP2012503621A5 true JP2012503621A5 (https=) | 2012-11-08 |
Family
ID=39952267
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011528309A Pending JP2012503621A (ja) | 2008-09-25 | 2009-09-22 | 生物活性プレチューブリシンおよびその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8791098B2 (https=) |
| EP (2) | EP2174947A1 (https=) |
| JP (1) | JP2012503621A (https=) |
| CA (1) | CA2738091A1 (https=) |
| WO (1) | WO2010034724A1 (https=) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5149620B2 (ja) | 2004-07-23 | 2013-02-20 | エンドサイト，インコーポレイテッド | ２価リンカーおよびその結合体 |
| CN104127878A (zh) | 2007-03-14 | 2014-11-05 | 恩多塞特公司 | 结合配体连接的微管溶素递药缀合物 |
| US9877965B2 (en) | 2007-06-25 | 2018-01-30 | Endocyte, Inc. | Vitamin receptor drug delivery conjugates for treating inflammation |
| BRPI0812970A2 (pt) | 2007-06-25 | 2019-09-24 | Endocyte Inc | conjugados contendo espaçadores hidrofílicos |
| US8394922B2 (en) | 2009-08-03 | 2013-03-12 | Medarex, Inc. | Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof |
| EP2409983A1 (en) | 2010-07-19 | 2012-01-25 | Leibniz-Institut für Pflanzenbiochemie (IPB) | Tubulysin analogues |
| WO2012171020A1 (en) | 2011-06-10 | 2012-12-13 | Mersana Therapeutics, Inc. | Protein-polymer-drug conjugates |
| US10080805B2 (en) | 2012-02-24 | 2018-09-25 | Purdue Research Foundation | Cholecystokinin B receptor targeting for imaging and therapy |
| US20140080175A1 (en) | 2012-03-29 | 2014-03-20 | Endocyte, Inc. | Processes for preparing tubulysin derivatives and conjugates thereof |
| US9981046B2 (en) | 2012-05-15 | 2018-05-29 | Concortis Biosystems, Corp., a wholly owned Subsidiary of Sorrento Therapeutics, Inc. | Drug-conjugates, conjugation methods, and uses thereof |
| PL2872157T3 (pl) | 2012-07-12 | 2020-07-13 | Hangzhou Dac Biotech Co., Ltd | Koniugaty wiążących komórkę cząsteczek ze środkami cytotoksycznymi |
| EP2908818A4 (en) | 2012-10-16 | 2016-07-13 | Endocyte Inc | CONJUGATES OF DRUG DELIVERY CONTAINING ARTIFICIAL AMINO ACIDS AND METHODS OF USE |
| US10131682B2 (en) | 2012-11-24 | 2018-11-20 | Hangzhou Dac Biotech Co., Ltd. | Hydrophilic linkers and their uses for conjugation of drugs to a cell binding molecules |
| CA2892863C (en) | 2012-12-10 | 2022-03-15 | Mersana Therapeutics, Inc. | Polymeric scaffold based on phf for targeted drug delivery |
| WO2014093640A1 (en) | 2012-12-12 | 2014-06-19 | Mersana Therapeutics,Inc. | Hydroxy-polmer-drug-protein conjugates |
| RS56169B1 (sr) | 2013-02-14 | 2017-11-30 | Bristol Myers Squibb Co | Jedinjenja tubulisina, metode pripreme i primena |
| US20160022829A1 (en) * | 2013-03-14 | 2016-01-28 | Mersana Therapeutics, Inc. | Tubulysin compounds and conjugates thereof |
| WO2015057585A1 (en) * | 2013-10-14 | 2015-04-23 | Regents Of The University Of Minnesota | Therapeutic compounds |
| WO2015057876A1 (en) | 2013-10-15 | 2015-04-23 | Sorrento Therapeutics Inc. | Drug-conjugates with a targeting molecule and two different drugs |
| ES2826398T3 (es) | 2013-10-15 | 2021-05-18 | Seagen Inc | Enlazadores-fármacos pegilados para una mejor farmacocinética de los conjugados ligando-fármaco |
| CA2938919C (en) | 2014-02-28 | 2020-12-29 | Hangzhou Dac Biotech Co., Ltd | Charged linkers and their uses for conjugation |
| US10077287B2 (en) | 2014-11-10 | 2018-09-18 | Bristol-Myers Squibb Company | Tubulysin analogs and methods of making and use |
| EP3250238B1 (en) | 2015-01-28 | 2022-06-01 | Sorrento Therapeutics, Inc. | Antibody drug conjugates |
| HK1248069A1 (zh) * | 2015-02-25 | 2018-10-12 | William Marsh Rice University | 去乙酰氧基微管溶素h及其类似物 |
| FI3319936T3 (fi) | 2015-07-12 | 2026-03-12 | Hangzhou Dac Biotech Co Ltd | Silloituslinkkereitä soluun sitoutuvien molekyylien konjugoimiseksi |
| US9839687B2 (en) | 2015-07-15 | 2017-12-12 | Suzhou M-Conj Biotech Co., Ltd. | Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule |
| US11793880B2 (en) | 2015-12-04 | 2023-10-24 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| CN108367043A (zh) | 2015-12-04 | 2018-08-03 | 西雅图基因公司 | 季铵化的微管溶素化合物的缀合物 |
| KR20180134351A (ko) | 2016-03-25 | 2018-12-18 | 시애틀 지네틱스, 인크. | 페길화된 약물-링커 및 그의 중간체의 제조를 위한 공정 |
| CA3042442C (en) | 2016-11-14 | 2024-01-02 | Hangzhou Dac Biotech Co., Ltd | Conjugation linkers, cell binding molecule-drug conjugates containing the linkers, methods of making and uses of such conjugates with the linkers |
| AU2018237683A1 (en) | 2017-03-24 | 2019-10-31 | Seagen Inc. | Process for the preparation of glucuronide drug-linkers and intermediates thereof |
| US11274124B2 (en) | 2017-11-29 | 2022-03-15 | William Marsh Rice University | Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith |
| MA53765B2 (fr) | 2018-12-21 | 2025-04-30 | Regeneron Pharmaceuticals, Inc. | Tubulysines et conjugués tubulysines-protéines |
| JP2022540395A (ja) | 2019-06-29 | 2022-09-15 | ハンジョウ ディーエーシー バイオテック シーオー．，エルティディ． | 細胞結合性分子－チューブリシン誘導体共役体及びその調製方法 |
| CN111647040B (zh) * | 2020-05-11 | 2022-02-22 | 深圳市老年医学研究所 | 一种天然活性多肽Tubulysin U的制备方法 |
| CN117980327A (zh) | 2021-11-03 | 2024-05-03 | 杭州多禧生物科技有限公司 | 抗体的特异性偶联 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10254439A1 (de) * | 2002-11-21 | 2004-06-03 | GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) | Tubulysine, Herstellungsverfahren und Tubulysin-Mittel |
| US20100047841A1 (en) * | 2007-02-27 | 2010-02-25 | University Of Pittsburgh-Of The Commonwealth System Of Higher Education | Synthesis of desacetoxytubulysin h and analogs thereof |
-
2008
- 2008-09-25 EP EP08165147A patent/EP2174947A1/en not_active Withdrawn
-
2009
- 2009-09-22 WO PCT/EP2009/062282 patent/WO2010034724A1/en not_active Ceased
- 2009-09-22 JP JP2011528309A patent/JP2012503621A/ja active Pending
- 2009-09-22 EP EP09783296A patent/EP2331559A1/en not_active Withdrawn
- 2009-09-22 CA CA2738091A patent/CA2738091A1/en not_active Abandoned
- 2009-09-22 US US13/120,497 patent/US8791098B2/en not_active Expired - Fee Related
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